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3-Aminothiophene-2-acylhydrazones: non-toxic, analgesic and anti-inflammatory lead-candidates.

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  • معلومة اضافية
    • المصدر:
      Publisher: MDPI Country of Publication: Switzerland NLM ID: 100964009 Publication Model: Electronic Cited Medium: Internet ISSN: 1420-3049 (Electronic) Linking ISSN: 14203049 NLM ISO Abbreviation: Molecules Subsets: MEDLINE
    • بيانات النشر:
      Original Publication: Basel, Switzerland : MDPI, c1995-
    • الموضوع:
      Analgesics/*chemistry ; Anti-Inflammatory Agents/*chemistry ; Hydrazones/*chemistry; Analgesics/therapeutic use ; Animals ; Anti-Inflammatory Agents/therapeutic use ; Arthritis/drug therapy ; Male ; Mice
    • نبذة مختصرة :
      Different chemotypes are described as anti-inflammatory. Among them the N-acylhydrazones (NAH) are highlighted by their privileged structure nature, being present in several anti-inflammatory drug-candidates. In this paper a series of functionalized 3-aminothiophene-2-acylhydrazone derivatives 5a-i were designed, synthesized and bioassayed. These new derivatives showed great anti-inflammatory and analgesic potency and efficacy. Compounds 5a and 5d stand out in this respect, and were also active in CFA-induced arthritis in rats. After daily treatment for seven days with 5a and 5d (50 µmol/Kg), by oral administration, these compounds were not renal or hepatotoxic nor immunosuppressive. Compounds 5a and 5d also displayed good drug-scores and low risk toxicity calculated in silico using the program OSIRIS Property Explorer.
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    • الرقم المعرف:
      0 (Analgesics)
      0 (Anti-Inflammatory Agents)
      0 (Hydrazones)
    • الموضوع:
      Date Created: 20140624 Date Completed: 20150109 Latest Revision: 20231004
    • الموضوع:
      20231215
    • الرقم المعرف:
      PMC6271570
    • الرقم المعرف:
      10.3390/molecules19068456
    • الرقم المعرف:
      24955640